天然存在的七肽[甲硫氨酸]脑啡肽-精氨酸6-苯丙氨酸7的镇痛活性。
Analgesic activity of the naturally occurring heptapeptide [Met]enkephalin-Arg6-Phe7.
作者信息
Inturrisi C E, Umans J G, Wolff D, Stern A S, Lewis R V, Stein S, Udenfriend S
出版信息
Proc Natl Acad Sci U S A. 1980 Sep;77(9):5512-4. doi: 10.1073/pnas.77.9.5512.
Abstract
[Met]Enkephalin-Arg6-Phe7 is an opiate-like peptide normally found in the the adrenal gland and brain that has analgesic (antinociceptive) activity when administered directly into the cerebral ventricles of mice. On a molar basis, [Met]-enkephalin-Arg6-Phe7, with a median effective dose (ED50) of 38.5 nmol/mouse, is 8 times more potent than [Met]enkephalin. As with [Met]enkephalin, analgesic activity is blocked by naloxone and intravenous administration does not produce characteristic opiate effects in tests for analgesic, antidiuretic, or antidiarrheal activity. These findings suggest that [Met]enkephalin-Arg6-Phe7 may be at least as important as the enkephalins in the postulated enkephalin system mediating pain and analgesia.
摘要
[甲硫氨酸]脑啡肽-精氨酸6-苯丙氨酸7是一种类似阿片样物质的肽，通常存在于肾上腺和大脑中，当直接注入小鼠脑室时具有镇痛（抗伤害感受）活性。以摩尔为基础，[甲硫氨酸]脑啡肽-精氨酸6-苯丙氨酸7的半数有效剂量（ED50）为38.5纳摩尔/小鼠，其效力是[甲硫氨酸]脑啡肽的8倍。与[甲硫氨酸]脑啡肽一样，纳洛酮可阻断其镇痛活性，并且静脉给药在镇痛、抗利尿或止泻活性测试中不会产生典型的阿片样物质效应。这些发现表明，在假定的介导疼痛和镇痛的脑啡肽系统中，[甲硫氨酸]脑啡肽-精氨酸6-苯丙氨酸7可能与脑啡肽至少同样重要。
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